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Cimetidine

消化

关键词消化 药物 癌症治疗

词汇介绍

拓展阅读

解析

cimetidine 英 [sɪ'metɪdɪn] 美 [sə'metədɪn]

释义   n. 甲氰咪胍,甲腈咪胍(抗消化性溃疡药)

例句   Methods: Three groups were treated with intragastric misoprostol, cimetidine, and placebo respectively.

方法:三组分别接受米索前列醇、甲氰咪胍和安慰剂治疗。


概述

西咪替丁(cimetidine)是一种H2受体阻断药(H2- receptor antagonists),体内分布广,可经胎盘到达胎儿体内,亦可透过血脑屏障,血浆蛋白结合率约19%。部分在体内代谢,代谢物及原形药经肾排出、肾功能不全时t1/2延长。此药口服易吸收,生物利用度约为75%、Tmax为1~2小时,血浆t1/2为2小时。单次给予治疗量作用约维持4小时。 药理作用与机制(1)抑制胃酸分泌;(2)免疫功能调节作用;(3)其他 西咪替丁能对抗组胺对离体心脏的正性肌力作用

Vitamin B12 Prevents Cimetidine-Induced Androgenic Failure and Damage to Sperm Quality in Rats复制标题

维生素B12预防西咪替丁诱导的大鼠雄激素衰竭和精子质量损伤

发表时间:2019-07-10

影响因子:3.6

作者: Flávia Luciana Beltrame

期刊:Front Endocrinol

Cimetidine, used as an anti-ulcer and adjuvant treatment in cancer therapy, causes disorders in the male reproductive tract, including steroidogenesis. However, its effect on sperm quality and male fertility has been poorly addressed. Since vitamin B12 has demonstrated to recover spermatogonia number and sperm concentration in cimetidine-treated rats, we evaluated the impact of cimetidine on sperm quality and fertility potential and whether vitamin B12 is able to prevent the harmful effect of this drug on steroidogenesis and sperm parameters. Adult male rats were treated  for 52 consecutive days as follows: cimetidine group(100 mg/kg of cimetidine),  cimetidine/vitamin B12 group (100 mg/kg of cimetidine + 3 µg vitamin B12), vitamin B12 group (3 µg vitamin B12) and control group (saline). Serum testosterone levels and immunofluorescence associated to western blot for detection of 17β-HSD6 were performed. Sperm morphology and motility, mitochondrial activity, acrosome integrity, DNA integrity by Comet assay, lipid peroxidation as well as fertility potential were analyzed in all groups. Apoptotic spermatids were also evaluated by caspase-3 immunohistochemistry. In the cimetidine-treated animals, reduced serum testosterone levels, weak 17β-HSD6 levels and impaired spermiogenesis were observed. Low sperm motility and mitochondrial activity were associated with high percentage of sperm tail abnormalities, and the percentage of spermatozoa with damaged acrosome and DNA fragmentation increased. MDA levels were normal in all groups, indicating that the cimetidine-induced changes are associated to androgenic failure. In conclusion, despite the fertility potential of rats was unaffected by the treatment, the sperm quality was significantly impaired.

译文

西咪替丁用作癌症治疗中的抗溃疡和辅助治疗,引起男性生殖道疾病,包括类固醇生成。然而,它对精子质量和男性生育能力的影响很难得到解决。由于维生素B12已被证实可以恢复西咪替丁治疗大鼠的精原细胞数量和精子浓度,我们评估了西咪替丁对精子质量和生育能力的影响以及维生素B12是否能够预防该药物对类固醇生成和精子参数的有害影响。成年雄性大鼠连续治疗52天:西咪替丁组(100 mg / kg西咪替丁),西咪替丁/维生素B12组(100 mg / kg西咪替丁+3μg维生素B12),维生素B12组(3μg维生素B12) )和对照组(生理盐水)。进行血清睾酮水平和与Western印迹相关的免疫荧光检测17β-HSD6。分析所有组的精子形态和运动,线粒体活性,顶体完整性,彗星试验的DNA完整性,脂质过氧化以及生育能力。还通过胱天蛋白酶-3免疫组织化学评估凋亡精子细胞。在西咪替丁治疗的动物中,观察到降低的血清睾酮水平,弱的17β-HSD6水平和受损的精子发生。低精子活力和线粒体活性与高比例的精子尾部异常有关,精子与顶体受损和DNA断裂的百分比增加。所有组的MDA水平均正常,表明西咪替丁诱导的变化与雄激素衰竭有关。总之,尽管大鼠的生育能力不受治疗影响,但精子质量明显受损。